MacPherson S E, Scott R C, Williams F M
Wolfson Unit of Clinical Pharmacology, University of Newcastle upon Tyne, UK.
Arch Toxicol. 1991;65(7):594-8. doi: 10.1007/BF01973722.
Metabolism of carbaryl by rat liver and skin post-mitochondrial fraction has been measured in the presence and absence of cofactors to promote different metabolic pathways. The metabolic capacity was compared with the metabolism of carbaryl during percutaneous absorption in a static skin diffusion system using a variety of receptor fluids. Carbaryl was metabolised by hydrolysis, and ring hydroxylation followed by conjugation to the glucuronide or sulphate with liver post-mitochondrial fraction. Using skin post-mitochondrial fraction only hydrolysis and conjugation were detected. No metabolism was seen during percutaneous absorption in vitro even with receptor fluids which maintain the skin tissue viability. Studies using post-mitochondrial fraction indicate the metabolic capacity of the tissue, whereas during absorption, rates of absorption and accessibility of substrate to the metabolising enzymes must be considered.
在有和没有辅助因子以促进不同代谢途径的情况下，已对大鼠肝脏和皮肤线粒体后组分对西维因的代谢进行了测定。在使用多种受体液的静态皮肤扩散系统中，将代谢能力与西维因经皮吸收过程中的代谢情况进行了比较。肝脏线粒体后组分可通过水解、环羟基化，然后与葡糖醛酸或硫酸盐结合来代谢西维因。仅使用皮肤线粒体后组分时，仅检测到水解和结合反应。即使使用能维持皮肤组织活力的受体液，在体外经皮吸收过程中也未观察到代谢现象。使用线粒体后组分进行的研究表明了组织的代谢能力，而在吸收过程中，必须考虑吸收速率和底物与代谢酶的可及性。
